解剖学和形态学
麻醉学
听力与言语-语言病理学
行为科学
心脏和心血管系统
细胞和组织工程学
临床神经病学
危重症监护医学
牙科,口腔外科和医学
皮肤病学
急诊医学
内分泌学和新陈代谢
肠胃学和肝脏学
老人病学和老年医学
卫生保健科学和服务
血液学
免疫学
传染病
综合和补充性医学
医学伦理学
医学信息学
医学实验室技术
医学,全科和内科
医学,法律
医学,研究和试验
神经系统科学
护理
营养学和饮食学
产科医学和妇科医学
肿瘤学
眼科学
整形外科学
耳鼻喉科学
病理学
儿科学
周围血管疾病
药理学和药剂学
生理学
基本医疗保健
精神病学
公共、环境和职业卫生
放射学,核医学和医学成像
康复学
生殖生物学
呼吸系统
风湿病学
运动科学
外科学
毒理学
热带医学
泌尿学和肾脏学
病毒学
老年医学
健康政策和服务
心理学,临床
abstract::Recent progress in peptide synthesis simplified the synthesis of multiple N-methylation of peptides. To evaluate how multiple N-methylation affects the bioavailability of peptides, a poly alanine cyclic hexapeptide library (n = 54), varying in the number of N-methyl (N-Me) groups (1-5 groups) and their position, was s...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp1003306
更新日期:2011-04-04 00:00:00
abstract::Recent developments in pharmaceutical technology have facilitated the design and production of modified release formulas for drugs whose physical, chemical or biological properties impede release and thus might compromise their efficacy or safety. One such drug is morphine, whose short half-life requires repeated dose...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp200019q
更新日期:2011-04-04 00:00:00
abstract::This paper develops a structure-activity relationship understanding of the way in which surfactant-like dendrons with hydrophilic spermine surface groups and a variety of lipophilic units at their focal points can self-assemble and subsequently bind to DNA with high affinity. The choice of functional group at the foca...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100260c
更新日期:2011-04-04 00:00:00
abstract::Within the immune system there is an exquisite ability to discriminate between "self" and "non-self" that is orchestrated by antigen-specific T lymphocytes. Genomic plasticity enables differentiation of naive CD4+ T lymphocytes into either regulatory cells (Treg) that express the transcription factor Foxp3 and activel...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100203a
更新日期:2011-02-07 00:00:00
abstract::Viral nanotechnology is an emerging and highly interdisciplinary field in which viral nanoparticles (VNPs) are applied in diverse areas such as electronics, energy and next-generation medical devices. VNPs have been developed as candidates for novel materials, and are often described as "programmable" because they can...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp100225y
更新日期:2011-02-07 00:00:00
abstract::Studies were conducted to develop antibody- and fluorescence-labeled superparamagnetic iron oxide nanoparticle (SPIO) nanotheranostics for magnetic resonance imaging (MRI) and fluorescence imaging of cancer cells and pH-dependent intracellular drug release. SPIO nanoparticles (10 nm) were coated with amphiphilic polym...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100273t
更新日期:2010-12-06 00:00:00
abstract::2-Methoxyestradiol (2MeO-E2) is an endogenous metabolite of estrogen which was initially considered to be inactive. During the last few decades it has been shown that 2MeO-E2 is a promising anticancer drug. In vitro experiments have demonstrated that it has several anticancer activities, and potential to alleviate hyp...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章,评审
doi:10.1021/mp100190f
更新日期:2010-12-06 00:00:00
abstract::In vivo peptide inhibition of tumor suppressor p53 binding to the protein MDM2 is hampered by inefficient delivery of the peptide. Our approach to couple a hydrophobic lipid-like tail on the inhibitory peptide p53(14-29) allowed its intracellular delivery in vitro, in a panel of different cell lines. The constructed c...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100193h
更新日期:2010-12-06 00:00:00
abstract::It is difficult to predict the first-pass effect in the human intestine due to a lack of scaling factors for correlating in vitro and in vivo data. We have quantified cytochrome P450/3A4 (CYP3A4) and two ABC transporters, P-glycoprotein (P-gp, ABCB1) and the breast cancer resistant protein BCRP (ABCG2), throughout the...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100015x
更新日期:2010-10-04 00:00:00
abstract::A series of poorly soluble BCS class II compounds with "grease ball" characteristics were assessed for solubility and dissolution rate in biorelevant dissolution media (BDM) with the purpose of investigating which molecular structures gain most in solubility when dissolved under physiologically relevant conditions. Th...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100049m
更新日期:2010-10-04 00:00:00
abstract::Oncolytic adenoviruses rank among the most promising innovative agents in cancer therapy. We examined the potential of boosting the efficacy of the oncolytic adenovirus dl520 by associating it with magnetic nanoparticles and magnetic-field-guided infection in multidrug-resistant (MDR) cancer cells in vitro and upon in...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100123t
更新日期:2010-08-02 00:00:00
abstract::Antiviral drugs often suffer from poor intestinal permeability, preventing their delivery via the oral route. The goal of this work was to enhance the intestinal absorption of the low-permeability antiviral agents zanamivir heptyl ester (ZHE) and guanidino oseltamivir (GO) utilizing an ion-pairing approach, as a criti...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100050d
更新日期:2010-08-02 00:00:00
abstract::Photodynamic therapy (PDT) is a light-induced chemical reaction that produces localized tissue damage for the treatment of cancers and other nonmalignant conditions. The activation of photosensitizers in a target tissue is accomplished with a specific light source in the presence of molecular oxygen. In the clinic, pa...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100060v
更新日期:2010-08-02 00:00:00
abstract::The Biopharmaceutical Classification System (BCS) guidance issued by the FDA allows waivers for in vivo bioavailability and bioequivalence studies for immediate-release (IR) solid oral dosage forms only for BCS class I drugs. However, a number of drugs within BCS class III have been proposed to be eligible for biowaiv...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100053q
更新日期:2010-08-02 00:00:00
abstract::This research determined the uptake of individual components of topically applied microemulsions into the stratum corneum (SC) and assessed their molecular effects on skin barrier function. The microemulsions comprised oleic acid, Tween20, Transcutol and water. The effects of selected formulations, and of the individu...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp100068s
更新日期:2010-08-02 00:00:00
abstract::The Flory-Huggins interaction parameter has been shown to be useful in predicting the thermodynamic miscibility of a polymer and a small molecule in a binary mixture. In the present paper, this concept was extended and evaluated to determine whether or not the Flory-Huggins interaction parameter can be applied to smal...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900304p
更新日期:2010-06-07 00:00:00
abstract::The need for an efficacious and safe oral anticoagulant that does not require monitoring has been largely unmet. Many efforts have centered on preparing orally available heparin to improve patient compliance. In this study, novel orally active heparin derivatives (LHD), i.e. low molecular weight heparin (LMWH) conjuga...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900319k
更新日期:2010-06-07 00:00:00
abstract::HEPES has been widely employed as an organic buffer agent in cell culture medium as well as uptake and transport experiments in vitro. However, concentrations of HEPES used in such studies vary from one laboratory to another. In this study, we investigated the effect of HEPES on the uptake and bidirectional transport ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900193e
更新日期:2010-04-05 00:00:00
abstract::Constitutively activated signal transducer and activator of transcription-3 (STAT3) in tumor and dendritic cells (DCs) plays a critical role in tumor-induced immunosuppression. This is considered a major challenge in effective immunotherapy of cancer. Herein we describe the development of a polymeric nanocarrier for t...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900145g
更新日期:2010-04-05 00:00:00
abstract::Polymeric micelles are emerging as a highly integrated nanoplatform for cancer targeting, drug delivery and tumor imaging applications. In this study, we describe a multifunctional micelle (MFM) system that is encoded with a lung cancer-targeting peptide (LCP), and encapsulated with superparamagnetic iron oxide (SPIO)...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp9001393
更新日期:2010-02-01 00:00:00
abstract::Ipratropium bromide, an anticholinergic drug used for the treatment of asthma and chronic obstructive pulmonary disease, has low oral bioavailability, but systemic exposure, superior to oral administration, can be achieved by inhalation. Therefore, we investigated the pulmonary absorption mechanism of ipratropium usin...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900206j
更新日期:2010-02-01 00:00:00
abstract::Nonsteroidal anti-inflammatory drugs (NSAIDs) can inhibit cell growth and metastasis, and induce cell apoptosis in cancerous cells. They have been shown to reduce incidence and mortality of gastric cancer by an unknown mechanism. NSAIDs often exert their effects by Cox-2 inhibition, and Cox-2 is overexpressed in gastr...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900189x
更新日期:2010-02-01 00:00:00
abstract::Targeted therapies are emerging as a preferred strategy for treatment of cancer and other diseases. To evaluate the effect of high affinity receptors on the rate and extent of tumor penetration of receptor-targeted drugs, we have characterized the kinetics of folate-rhodamine uptake by folate receptor (FR)-expressing ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900158d
更新日期:2009-11-01 00:00:00
abstract::Poly(ethylcyanoacrylate) (PECA) nanoparticles containing the bioactive d-Lys(6)-GnRH were manufactured by an in situ interfacial polymerization process using a w/o-microemulsion template containing the peptide in the dispersed aqueous pseudophase of the microemulsion. Polymeric nanoparticles were characterized using P...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900043e
更新日期:2009-09-01 00:00:00
abstract::We evaluated the chemical and enzymatic stabilities of prodrugs containing methoxy, ethoxy and propylene glycol linkers in order to find a suitable linker for prodrugs of carboxylic acids with amino acids. l-Valine and l-phenylalanine prodrugs of model compounds (benzoic acid and phenyl acetic acid) containing methoxy...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900084v
更新日期:2009-09-01 00:00:00
abstract::The objective was to determine the disposition of polymer nanoparticles and an associated, lipophilic, model "active" component on and within the skin following topical application. Polystyrene and poly(methyl methacrylate) nanoparticles containing covalently bound fluorescein methacrylate and dispersed Nile Red were ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp9001188
更新日期:2009-09-01 00:00:00
abstract::The antiviral drug tenofovir (TFV) is orally administered as the fumarate salt of its disoproxil prodrug (TFV disoproxil fumarate (TDF)). TFV is a dianion at physiological pH and, as a result, has poor lipid membrane permeability. Administration of the lipophilic and cell-permeable prodrug, TFV disoproxil, enhances th...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900036s
更新日期:2009-07-01 00:00:00
abstract::Effective delivery is a critical issue in the use of conventional free drugs. Studies on the structure-function relationship of a therapeutic antibody-derived candidacidal decapeptide (killer peptide, KP) revealed its ability to spontaneously and reversibly self-assemble in an organized network of fibril-like structur...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900024z
更新日期:2009-05-01 00:00:00
abstract::We report on the fabrication and characterization of dry hybrid lipid-silica nanoparticle based microcapsules with an internal porous matrix structure for encapsulation of poorly soluble drugs, and their delivery properties (in vitro release and lipolysis and in vivo pharmacokinetics demonstrated for indomethacin as a...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp900063t
更新日期:2009-05-01 00:00:00
abstract::Peptide nucleic acids have a number of features that make them an ideal platform for the development of in vitro biological probes and tools. Unfortunately, their inability to pass through membranes has limited their in vivo application as diagnostic and therapeutic agents. Herein, we describe the development of catio...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800199w
更新日期:2009-03-01 00:00:00
abstract::Dry powders from aqueous dispersions, formed by antisolvent precipitation, dissolved to form solutions with supersaturation values up to 12 in 10 min at pH 6.8 with sodium dodecyl sulfate micelles. Itraconazole/hydroxypropylmethylcellulose (HPMC) aqueous particle dispersions were salt flocculated and filtered to produ...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800106a
更新日期:2009-03-01 00:00:00
abstract::Selective ligands to the peripheral benzodiazepine receptor (PBR) may induce apoptosis and cell cycle arrest. An overexpression of PBR in certain cancers allowed us to consider the use of highly selective ligands to PBR for receptor-mediated drug targeting to tumors. With this in mind, we prepared PBR-targeted nanopar...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800158c
更新日期:2009-03-01 00:00:00
abstract::The purpose of this study was to investigate the role of P-gp efflux in the in vivo intestinal absorption process of BCS class III P-gp substrates, i.e. high-solubility low-permeability drugs. The in vivo permeability of two H (2)-antagonists, cimetidine and famotidine, was determined by the single-pass intestinal per...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800088f
更新日期:2009-01-01 00:00:00
abstract::The aim of the research work was to develop and characterize a concanavalin-A (Con-A) conjugated gastroretentive multiparticulate delivery system of clarithromycin (CM) for the effective treatment of colonization of Helicobacter pylori (H. pylori). Ethylcellulose (EC) microspheres containing CM were prepared using emu...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800193n
更新日期:2009-01-01 00:00:00
abstract::Amorphous solids and crystalline salts are both of interest as a means of improving the dissolution characteristics and apparent solubility of poorly water soluble active pharmaceutical ingredients which have low bioavailability in humans. The theory and selection of both crystalline drug substance salt forms and amor...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp8000342
更新日期:2008-11-01 00:00:00
abstract::Amorphous solid dispersions (ASD) of a poorly soluble water-soluble VR1 antagonist (AMG 517) were explored for improving physical stability and in vivo exposure. AMG 517 was incorporated at 15 or 50 wt % into polymeric microparticles of hydroxypropyl methylcellulose acetate succinate (HPMCAS) and hydroxypropyl methylc...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800061r
更新日期:2008-11-01 00:00:00
abstract::The transfection activity and the phase behavior of two novel cationic O-alkyl-phosphatidylcholines, 1,2-dioleoyl- sn-glycero-3-hexylphosphocholine (C6-DOPC) and 1,2-dierucoyl- sn-glycero-3-ethylphosphocholine (di22:1-EPC), have been examined with the aim of more completely understanding the mechanism of lipid-mediate...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800011e
更新日期:2008-09-01 00:00:00
abstract::The synthesis and biodistribution of three triazine dendrimers differing in PEGylation are described. Dendrimers 1, 2, and 3 are derived from a common intermediate, dendrimer 4, and vary in molecular mass from 11 to 73 kDa as a result of PEGylation with multiple (theoretically, 16) PEG groups of 0.6, 2, and 5 kDa, res...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp8000292
更新日期:2008-07-01 00:00:00
abstract::Multidrug resistance (MDR), a major obstacle to successful cancer chemotherapy, may be induced by amplification of the MDR1 gene and overexpression of the P-glycoprotein (P-gp), which acts as drug efflux pump decreasing intracellular drug accumulation. In this study, an antisense oligodeoxynucleotide--doxorubicin conj...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp800001j
更新日期:2008-07-01 00:00:00
abstract::Reversible aqueous lipidization (REAL) at the interdisulfide bond has been shown to improve the deliverability of some peptide drugs. Recently, we developed a nonreversible aqueous lipidization method targeted at the interdisulfide bond of salmon calcitonin (sCT). The resultant derivative had comparable hypocalcemic a...
journal_title:Molecular pharmaceutics
pub_type: 杂志文章
doi:10.1021/mp8000167
更新日期:2008-07-01 00:00:00